Concepts and Case Studies in Chemical Biology

Herbert Waldmann obtained his PhD in organic chemistry from the University of Mainz, Germany, in 1985 working with Professor H. Kunz, after which he completed a postdoctoral appointment with Professor G. Whitesides at Harvard University (USA). He was appointed as Professor of Organic Chemistry at the University of Bonn (1991), full Professor of Organic Chemistry at the University of Karlsruhe (1993), and Director at the Max-Planck-Institute of Molecular Physiology Dortmund and Professor of Organic Chemistry at the University of Dortmund, Germany, in 1999. He has received numerous awards, e.g. the Otto-Bayer-Award (2001), the Max Bergmann Medal (2003), and recently the Emil-Fischer-Prize (2012). His research interests lie in bioactive compound development, target identification, and the chemical biology of Ras proteins.

Petra Janning studied chemistry at the University of Münster, Germany, and did her PhD thesis at the Institute for Analytical Sciences in Dortmund, Germany in 1995. After different positions where she worked in the area of analytical chemistry and on the borderline between chemistry and biology she joined the Max-Planck-Institute of Molecular Physiology, Dortmund, in the department of Professor H. Waldmann, where she is currently working. She is responsible for the Bioorganic Practical Course and the analytics in the department. She focused her work on mass spectrometry based methods in proteome research, in particular in target protein identification of small molecules.

1. Real-Time and Continuous Sensors of Protein Kinase Activity Utilizing Chelation-Enhanced Fluorescence

2. FLiK and FLiP: Direct Binding Assays for the Identification of Stabilizers of Inactive Kinase and Phosphatase Conformations

3. Strategies for Designing Specific Protein Tyrosine Phosphatase Inhibitors and their Intracellular Activation

4. Design and Application of Chemical Probes for Protein Serine/Threonine Phosphatase Activation

5. Autophagy: Assays and Small Molecule Modulators

6. Elucidation of Protein Function by Chemical Modification

7. Inhibition of Oncogenic K-Ras Signaling by Targeting K-Ras-PDEDelta Interaction

8. Development of Acyl Protein Thioesterase
1 (APT1) Inhibitor Palmostatin B that Revert Unregulated H/N-Ras Signaling

9. Functional Analysis of Host-Pathogen Posttranslational Modification Crosstalk of Rab Proteins

10. Chemical Biology Approach to Suppression of Statin-Induced Muscle Toxicity

11. A Target Identification System Based on MorphoBase, ChemProteoBase, and Photo-Crosslinking Beads

12. Activity-Based Proteasome Profiling in Medicinal Chemistry and Chemical Biology

13. Rational Design of Activity-Based Retaining Beta-Exoglucosidase Probes

14. Modulation of ClpP Protease Activity: From Antibiotics to Anti-Virulence

15. Affinity-Based Isolation of Molecular Targets of Clinically used Drugs

16. Identification of the Targets of Natural Product-Inspired Mitotic Inhibitors

17. Finding a Needle in a Haystack. Identification of Tankyrase a Novel Therapeutic Target of the Wnt Pathway using Chemical Genetics

18. The Identification of the Molecular Reporter of the Plant Hormone Abscisic Acid

19. Chemical Biology in Plants: Finding New Connections between Pathways using the Small Molecule Sortin
1

20. Selective Targeting of Protein Interactions Mediated by BET Bromodomains

21. The Impact of Distant Polypharmacology in the Chemical Biology of PARPs

22. Splicing Inhibitors: From Small Molecule to RNA Metabolism

23. Photochemical Control of Gene Function in Zebrafish Embryos with Light-Activated Morpholinos

24. Life Cell Imaging of mRNA using PNA FIT-Probes

25. Targeting the Transcriptional Hub Beta-Catenin using Stapled Peptides

26. Diversity Oriented Synthesis: Developing New Chemical Tools to Probe and Modulate Biological Systems

27. Scaffold Diversity Synthesis with Branching Cascades Strategy